MAGL-IN-4

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MAGL-IN-4 是一种单酰基甘油脂肪酶 (MAGL) 抑制剂，用于治疗中枢神经系统相关疾病。

MAGL-IN-4 is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.(In Vitro):MAGL-IN-4 showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption and blood-brain barrier penetration.(In Vivo):MAGL-IN-4 showed significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice.

MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL.MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA).

MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice.

His121 ARG57

Metabolic Enzyme/Protease

Lipase

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2135785-20-3

364.82

C18H21ClN2O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (274.11 mM)

O=C(OC1)N[C@@]21C[C@@H](C(N3CC(OCC4=CC=C(C)C(Cl)=C4)C3)=O)C2

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(-20℃)

With Ice Pack

≥ 2 years